Poly(amidoamine) dendrimer-methotrexate conjugates: the mechanism of interaction with folate binding protein.

abstract：:The biodistribution of dendronized iron oxides, NPs10@D1_DOTAGA and melanin-targeting NPs10@D1_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [177Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized nanoparticles (DPs) and hepatobil...

journal_title：Molecular pharmaceutics

authors： Bordeianu C,Parat A,Piant S,Walter A,Zbaraszczuk-Affolter C,Meyer F,Begin-Colin S,Boutry S,Muller RN,Jouberton E,Chezal JM,Labeille B,Cinotti E,Perrot JL,Miot-Noirault E,Laurent S,Felder-Flesch D

更新日期：2018-02-05 00:00:00

abstract：:Human epidermal growth factor receptor 2 (HER2) is a biomarker in breast cancer, and its overexpression is required to initiate therapies using HER2-targeted antibodies. Although trastuzumab is one of the most effective therapeutic antibodies in HER2-overexpressing breast cancer, a significant number of patients do no...

journal_title：Molecular pharmaceutics

authors： Pereira PMR,Ragupathi A,Shmuel S,Mandleywala K,Viola NT,Lewis JS

更新日期：2020-01-06 00:00:00

abstract：:Organic anion transporting polypeptide (OATP) 1B1 plays an important role in the hepatic uptake of various drugs. Because OATP1B1 is a site of drug-drug interactions (DDIs), evaluating the inhibitory potential of drug candidates on OATP1B1 is required during drug development. For establishing a highly sensitive, high-...

journal_title：Molecular pharmaceutics

authors： Izumi S,Nozaki Y,Komori T,Takenaka O,Maeda K,Kusuhara H,Sugiyama Y

更新日期：2016-02-01 00:00:00

abstract：:We report herein on the preparation of thermoresponsive hydrogels by taking advantage of the interaction of cyclodextrins (CDs) and a hydrophobically modified polymer. A hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC) gel formed thermoresponsive hydrogels when small amounts of α-CD were added to the s...

journal_title：Molecular pharmaceutics

authors： Iohara D,Okubo M,Anraku M,Uramatsu S,Shimamoto T,Uekama K,Hirayama F

更新日期：2017-08-07 00:00:00

abstract：:Polymer therapeutics offer potential benefits in the treatment of multidrug resistant (MDR) infections; affording targeted delivery of biologically active agents to the site of inflammation, potential decreases in systemic toxicity, and the retention of antimicrobial activity at the target site. As a prototype model, ...

journal_title：Molecular pharmaceutics

authors： Ferguson EL,Azzopardi E,Roberts JL,Walsh TR,Thomas DW

更新日期：2014-12-01 00:00:00

abstract：:The drug-induced accumulation of phospholipids in lysosomes of various tissues is predominantly observed in regular repeat dose studies, often after prolonged exposure, and further investigated in mechanistic studies prior to candidate nomination. The finding can cause delays in the discovery process inflicting high c...

journal_title：Molecular pharmaceutics

authors： Fusani L,Brown M,Chen H,Ahlberg E,Noeske T

更新日期：2017-12-04 00:00:00

abstract：:The bicarbonate buffer capacity is usually considered in a phase-homogeneous system, at equilibrium, with no CO2 transfer between the liquid buffer phase and another phase. However, typically, an in vitro bicarbonate buffer-based system is a phase-heterogeneous system, as it entails continuously sparging (bubbling) th...

journal_title：Molecular pharmaceutics

authors： Al-Gousous J,Sun KX,McNamara DP,Hens B,Salehi N,Langguth P,Bermejo M,Amidon GE,Amidon GL

更新日期：2018-11-05 00:00:00

abstract：:Platinum(IV) complexes generally require reduction to reactive Pt(II) species to exert their chemotherapeutic activity. The process of reductive activation of (15)N-labeled (OC-6-43)-bis(acetato)diamminedichloridoplatinum(IV), in the presence of nicotinamide adenine dinucleotide (NADH) and horse heart cytochrome c (cy...

journal_title：Molecular pharmaceutics

authors： Lasorsa A,Stuchlíková O,Brabec V,Natile G,Arnesano F

更新日期：2016-09-06 00:00:00

abstract：:Improving the therapeutic index of anticancer agents is an enormous challenge. Targeting decreases the side effects of the therapeutic agents by delivering the drugs to the intended destination. Nanocarriers containing the nuclear localizing peptide sequences (NLS) translocate to the cell nuclei. However, the nuclear ...

journal_title：Molecular pharmaceutics

authors： Anajafi T,Yu J,Sedigh A,Haldar MK,Muhonen WW,Oberlander S,Wasness H,Froberg J,Molla MS,Katti KS,Choi Y,Shabb JB,Srivastava DK,Mallik S

更新日期：2017-06-05 00:00:00

abstract：:Nonviral gene delivery has seen limited clinical application due in part to the inefficiency with which most nonviral vehicles navigate the intracellular gene delivery pathway. One key problem is the inability of most DNA-packaging materials to release DNA and enable its efficient transcription. Thus, our aim was to d...

journal_title：Molecular pharmaceutics

authors： Larsen JD,Reilly MJ,Sullivan MO

更新日期：2012-05-07 00:00:00

abstract：:Gemcitabine (GEM), a first-line chemotherapy for pancreatic cancer undergoes rapid metabolism and develops chemoresistance after repeated administration. We previously demonstrated that the combination of GEM and miR-205 provides an effective therapeutic strategy to sensitize GEM-resistant pancreatic cancer cells. Sin...

journal_title：Molecular pharmaceutics

authors： Mondal G,Almawash S,Chaudhary AK,Mahato RI

更新日期：2017-09-05 00:00:00

abstract：:Selective ligands to the peripheral benzodiazepine receptor (PBR) may induce apoptosis and cell cycle arrest. An overexpression of PBR in certain cancers allowed us to consider the use of highly selective ligands to PBR for receptor-mediated drug targeting to tumors. With this in mind, we prepared PBR-targeted nanopar...

journal_title：Molecular pharmaceutics

authors： Musacchio T,Laquintana V,Latrofa A,Trapani G,Torchilin VP

更新日期：2009-03-01 00:00:00

abstract：:The barrier epithelia of the cornea and retina control drug and nutrient access to various compartments of the human eye. While ocular transporters are likely to play a critical role in homeostasis and drug delivery, little is known about their expression, localization and function. In this study, the mRNA expression ...

journal_title：Molecular pharmaceutics

authors： Dahlin A,Geier E,Stocker SL,Cropp CD,Grigorenko E,Bloomer M,Siegenthaler J,Xu L,Basile AS,Tang-Liu DD,Giacomini KM

更新日期：2013-02-04 00:00:00

abstract：:Effective delivery is a critical issue in the use of conventional free drugs. Studies on the structure-function relationship of a therapeutic antibody-derived candidacidal decapeptide (killer peptide, KP) revealed its ability to spontaneously and reversibly self-assemble in an organized network of fibril-like structur...

journal_title：Molecular pharmaceutics

authors： Pertinhez TA,Conti S,Ferrari E,Magliani W,Spisni A,Polonelli L

更新日期：2009-05-01 00:00:00

abstract：:The formulation of drug/polymer amorphous solid dispersions (ASDs) is one of the most successful strategies for improving the oral bioavailability of poorly soluble active pharmaceutical ingredients (APIs). Hot-melt extrusion (HME) is one method for preparing ASDs that is growing in importance in the pharmaceutical in...

journal_title：Molecular pharmaceutics

authors： Pisa E,Hughes LP,Wren SAC,Booth J,McCabe JF,Whittaker DTE,Mantle MD

更新日期：2020-06-01 00:00:00

abstract：:Formulation of a cocrystal into a solid pharmaceutical dosage form entails numerous processing steps during which there is risk of dissociation. In an effort to reduce the number of unit operations, we have attempted the in situ formation of an indomethacin-saccharin (INDSAC) cocrystal during high-shear wet granulatio...

journal_title：Molecular pharmaceutics

authors： Tanaka R,Duggirala NK,Hattori Y,Otsuka M,Suryanarayanan R

更新日期：2020-01-06 00:00:00

abstract：:Antiviral drugs often suffer from poor intestinal permeability, preventing their delivery via the oral route. The goal of this work was to enhance the intestinal absorption of the low-permeability antiviral agents zanamivir heptyl ester (ZHE) and guanidino oseltamivir (GO) utilizing an ion-pairing approach, as a criti...

journal_title：Molecular pharmaceutics

authors： Miller JM,Dahan A,Gupta D,Varghese S,Amidon GL

更新日期：2010-08-02 00:00:00

abstract：:By the combined use of powder and single-crystal X-ray diffraction, solid-state NMR, and molecular modeling, the crystal structures of two systems containing the unusually large tenapanor drug molecule have been determined: the free form, ANHY, and a dihydrochloride salt form, 2HCl. Dynamic nuclear polarization (DNP) ...

journal_title：Molecular pharmaceutics

authors： Nilsson Lill SO,Widdifield CM,Pettersen A,Svensk Ankarberg A,Lindkvist M,Aldred P,Gracin S,Shankland N,Shankland K,Schantz S,Emsley L

更新日期：2018-04-02 00:00:00

abstract：:L cells have attracted particular interest because of the pleiotropic effects of their secreted peptides (i.e., glucagon-like peptide (GLP) 1 and 2, peptide YY (PYY)). L cells express different G-protein-coupled receptors (GPCRs) that can be activated by endogenous ligands found in the gut lumen. We herein hypothesize...

journal_title：Molecular pharmaceutics

authors： Beloqui A,Alhouayek M,Carradori D,Vanvarenberg K,Muccioli GG,Cani PD,Préat V

更新日期：2016-12-05 00:00:00

abstract：:Peritoneal fibrosis (PF) is a common complication of long-term peritoneal dialysis (PD). It is considered as the main reason for dialysis inadequacy and PD withdrawal. Transforming growth factor beta (TGF-β) regulates the expression of stromal cell-derived factor 1 (SDF-1α) and its receptor C-X-C chemokine receptor ty...

journal_title：Molecular pharmaceutics

authors： Asifullah K,Zhou Z,He W,Gao K,Khan MW,Faisal R,Muhammad H,Sun M

更新日期：2019-06-03 00:00:00

abstract：:The human organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) are liver-enriched membrane transporters of major importance to hepatic uptake of numerous endogenous compounds, including bile acids, steroid conjugates, hormones, and drugs, including the 3-hydroxy-3-methylglutaryl Co-A reducta...

journal_title：Molecular pharmaceutics

authors： DeGorter MK,Ho RH,Leake BF,Tirona RG,Kim RB

更新日期：2012-04-02 00:00:00

abstract：:Abnormal extracellular deposition of β-amyloid (Aβ) is thought to play a key role in the pathogenesis of Alzheimer's disease (AD). Preventing Aβ-induced neurotoxicity has become a potential therapeutic approach to improve the onset and progression of AD. Here we report the synthesis of 1,1'-(biphenyl-4,4'-diyl)-bis(3-...

journal_title：Molecular pharmaceutics

authors： Zhu Y,Sun X,Gong T,He Q,Zhang Z

更新日期：2014-02-03 00:00:00

abstract：:Drug transporter expression and function at the blood-brain barrier is altered in Alzheimer's disease (AD). However, the impact of AD on the expression of transporters and metabolizing enzymes in peripheral tissues has received little attention. The current study evaluated the expression of drug transporters and metab...

journal_title：Molecular pharmaceutics

authors： Pan Y,Omori K,Ali I,Tachikawa M,Terasaki T,Brouwer KLR,Nicolazzo JA

更新日期：2018-09-04 00:00:00

abstract：:Genospheres are cationic lipid-nucleic acid nanoparticles prepared by the assembly of the lipids and nucleic acids from an aqueous/organic liquid monophase that independently dissolves the components, where the resultant particles are homogeneously sized (70-110 nm), with efficiently incorporated and protected DNA. In...

journal_title：Molecular pharmaceutics

authors： Hayes ME,Drummond DC,Hong K,Zheng WW,Khorosheva VA,Cohen JA,C O N 4th,Park JW,Marks JD,Benz CC,Kirpotin DB

更新日期：2006-11-01 00:00:00

abstract：:Despite advances in cancer therapies, glioblastoma multiforme treatment remains inefficient due to the brain-blood barrier (BBB) inhibitory activity and to the low temozolomide (TMZ) chemotherapeutic selectivity. To improve therapeutic outcomes, in this work we propose two strategies, (i) photodynamic therapy (PDT) as...

journal_title：Molecular pharmaceutics

authors： Pellosi DS,Paula LB,de Melo MT,Tedesco AC

更新日期：2019-03-04 00:00:00

abstract：:The foreign body reaction (FBR), one of the body's defense mechanisms against foreign materials, results in loss of implant biocompatibility. A popular strategy to prevent FBR is the constant release of dexamethasone in the tissue surrounding the implant. However, FBR prevention has not been sufficiently studied in la...

journal_title：Molecular pharmaceutics

authors： Kastellorizios M,Tipnis N,Papadimitrakopoulos F,Burgess DJ

更新日期：2015-09-08 00:00:00

abstract：:This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...

journal_title：Molecular pharmaceutics

authors： Jones SP,Gabrielson NP,Wong CH,Chow HF,Pack DW,Posocco P,Fermeglia M,Pricl S,Smith DK

更新日期：2011-04-04 00:00:00

abstract：:The reaction of singlet oxygen with water to form hydrogen peroxide was catalyzed by antibodies and has been termed as the antibody catalyzed water oxidation pathway (ACWOP) (Nieva and Wentworth, Trends Biochem. Sci. 2004, 29, 274-278; Nieva et al. Immunol. Lett. 2006, 103, 33-38). While conserved and buried tryptopha...

journal_title：Molecular pharmaceutics

authors： Sreedhara A,Lau K,Li C,Hosken B,Macchi F,Zhan D,Shen A,Steinmann D,Schöneich C,Lentz Y

更新日期：2013-01-07 00:00:00

abstract：:Heart transplantation (HT) is an effective treatment for end-stage heart disease. However, acute rejection (AR) is still the main cause of death within one year after HT. AR is an acute immune response mediated by T lymphocytes, mainly CD4+ T lymphocytes. This study innovatively develops a radiolabeled probe 99mTc-HYN...

journal_title：Molecular pharmaceutics

authors： Li H,Chen Y,Jin Q,Wu Y,Deng C,Gai Y,Sun Z,Li Y,Wang J,Yang Y,Lv Q,Zhang Y,An R,Lan X,Zhang L,Xie M

更新日期：2021-01-28 00:00:00

abstract：:A general, easy-to-implement strategy for mapping the structure of organic phases integrated in mesoporous silica drug delivery devices is presented. The approach based on a few straightforward solid-state NMR techniques has no limitations regarding concentrations of the active compounds and enables straightforward di...

journal_title：Molecular pharmaceutics

authors： Brus J,Albrecht W,Lehmann F,Geier J,Czernek J,Urbanova M,Kobera L,Jegorov A

更新日期：2017-06-05 00:00:00